Oxaliplatin (OXA) is a valuable and largely used cancer drug which induces a serious and intractable neuropathy. The lipoyl-homotaurine derivative (ADM_12) reverts in vivo OXA-induced neuropathy, and it is an effective antagonist of the nociceptive sensor channel TRPA1. Unprecedentedly, this safe analgesic showed a synergy with OXA in vitro and proved to inhibit CA IX, a relevant therapeutic target, clearly interfering with pancreatic cancer cells' aggressiveness.
Lipoyl-Homotaurine Derivative (ADM_12) Reverts Oxaliplatin-Induced Neuropathy and Reduces Cancer Cells Malignancy by Inhibiting Carbonic Anhydrase IX (CAIX) / Fragai, Marco; Comito, Giuseppina; Di Cesare Mannelli, Lorenzo; Gualdani, Roberta; Calderone, Vito; Louka, Alexandra; Richichi, Barbara; Francesconi, Oscar; Angeli, Andrea; Nocentini, Alessio; Gratteri, Paola; Chiarugi, Paola; Ghelardini, Carla; Tadini-Buoninsegni, Francesco; Supuran, Claudiu T; Nativi, Cristina. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 1520-4804. - STAMPA. - 60:(2017), pp. 9003-9011. [10.1021/acs.jmedchem.7b01237]
Lipoyl-Homotaurine Derivative (ADM_12) Reverts Oxaliplatin-Induced Neuropathy and Reduces Cancer Cells Malignancy by Inhibiting Carbonic Anhydrase IX (CAIX)
Fragai, Marco;Comito, Giuseppina;Di Cesare Mannelli, Lorenzo;Gualdani, Roberta;Calderone, Vito;Louka, Alexandra;Richichi, Barbara;Francesconi, Oscar;Angeli, Andrea;Nocentini, Alessio;Gratteri, Paola;Chiarugi, Paola;Ghelardini, Carla;Tadini-Buoninsegni, Francesco;Supuran, Claudiu T
;Nativi, Cristina
2017
Abstract
Oxaliplatin (OXA) is a valuable and largely used cancer drug which induces a serious and intractable neuropathy. The lipoyl-homotaurine derivative (ADM_12) reverts in vivo OXA-induced neuropathy, and it is an effective antagonist of the nociceptive sensor channel TRPA1. Unprecedentedly, this safe analgesic showed a synergy with OXA in vitro and proved to inhibit CA IX, a relevant therapeutic target, clearly interfering with pancreatic cancer cells' aggressiveness.
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Nativi etal_Text_JMedChem.pdf
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